公开(公告)号：US20070167435A1

公开(公告)日：2007-07-19

申请号：US11641175

申请日：2006-12-19

申请人： Mwangi Mutahi ,  Robert Aslanian ,  Michael Berlin ,  Christopher Boyce ,  Manuel de Lera Ruiz ,  Kevin McCormick ,  Daniel Solomon ,  Henry Vaccaro ,  Junying Zheng ,  Purakkattle Biju ,  Younong Yu ,  Wei Zhou ,  Xiaohong Zhu

发明人： Mwangi Mutahi ,  Robert Aslanian ,  Michael Berlin ,  Christopher Boyce ,  Manuel de Lera Ruiz ,  Kevin McCormick ,  Daniel Solomon ,  Henry Vaccaro ,  Junying Zheng ,  Purakkattle Biju ,  Younong Yu ,  Wei Zhou ,  Xiaohong Zhu

IPC分类号： A61K31/551 ,  A61K31/501 ,  A61K31/506 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D213/38 ,  C07D213/73 ,  C07D277/40 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D417/06 ,  C07D417/14 ,  C07D473/00

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.

摘要翻译： 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：M是CH或N; U和W各自为CH，或U和W中的一个为CH，另一个为N; X是键，亚烷基，-C（O） - ， - C（N-OR 5） - ， - （N -OR 5）-CH（R - （CH 3） - ， - CH（R 6） - ， - （N-OR 5） - ， - O - ， - 2 - ， - CH 2 O-或-S（O）0-2 - 。 Y是-O-， - （CH 2）2 - ， - C（-O） - ， - C（-NOR 7） - 或-SO <0-2 - ; - Z是一个键，任选取代的被杂原子或杂环基中断的亚烷基或亚烷基; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基或苯并咪唑基或其衍生物; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，糖尿病，肥胖，肥胖相关病症，代谢综合征和认知缺陷障碍的组合物和方法。

公开(公告)号：US08003624B2

公开(公告)日：2011-08-23

申请号：US11705683

申请日：2007-02-13

申请人： Kevin D. McCormick ,  Christopher W. Boyce ,  Younong Yu

发明人： Kevin D. McCormick ,  Christopher W. Boyce ,  Younong Yu

IPC分类号： A01N57/00 ,  C07D215/38 ,  C07D209/04 ,  C07D223/16

CPC分类号： C07D403/02 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了作为α2C肾上腺素能受体激动剂抑制剂的新一类中和体，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及 使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。

公开(公告)号：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

申请人： Amjad ALI ,  Michael Man-Chu LO ,  Yeon-Hee LIM ,  Andrew STAMFORD ,  Rongze KUANG ,  Paul TEMPEST ,  Younong YU ,  Michael BERLIN ,  Pauline TING ,  Gang ZHOU ,  Tao YU ,  Christopher BOYCE ,  Joseph Michael KELLY ,  Jayaram TAGAT ,  Junying ZHENG ,  Xianhai HUANG ,  Wei ZHOU ,  Jae-Hun KIM ,  Nicolas ZORN ,  Dong XIAO ,  Gioconda V. GALLO ,  Walter WON ,  Heping WU ,  Rajan ANAND ,  MERCK SHARP & DOHME CORP.

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC分类号： C07D487/04 ,  C07D487/18 ,  C07D487/08 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

摘要翻译： 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US07671212B2

公开(公告)日：2010-03-02

申请号：US11017505

申请日：2004-12-20

申请人： Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Junying Zheng ,  Purakkattle J. Biju ,  Younong Yu ,  Jianhua Chao ,  Gaifa Lai ,  Minglang Wu

发明人： Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Junying Zheng ,  Purakkattle J. Biju ,  Younong Yu ,  Jianhua Chao ,  Gaifa Lai ,  Minglang Wu

IPC分类号： A61K31/425 ,  C07D275/03

CPC分类号： C07D275/03 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

摘要翻译： 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 D和E是不同的组，其中一个是N，另一个是CR 50。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和心脏再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎症性疼痛和神经性疼痛）。

公开(公告)号：US20150361098A1

公开(公告)日：2015-12-17

申请号：US14655648

申请日：2013-12-20

申请人： Amjad ALI ,  Michael Man-Chu LO ,  Yeon-Hee LIM ,  Andrew STAMFORD ,  Rongze KUANG ,  Paul TEMPEST ,  Younong YU ,  Xianhai HUANG ,  Timothy J. HENDERSON ,  Jae-Hun KIM ,  Christopher BOYCE ,  Pauline TING ,  Junying ZHENG ,  Edward METZGER ,  Nicolas ZORN ,  Dong XIAO ,  Gloconda GALLO ,  Walter WON ,  Heping WU ,  MERCH SHARP & DOHME CORP.

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC分类号： C07D519/00 ,  C07D487/04

CPC分类号： C07D519/00 ,  C07D487/04

摘要： Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

摘要翻译： 公开了式G1（结构表示）的化合物：其中“RG3”“Rd1”至“Rd4”，“n”，“m”，“p”，“W”，“X”，“Y”和“Z “在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US20080090823A1

公开(公告)日：2008-04-17

申请号：US11861870

申请日：2007-09-26

申请人： Purakkattle Biju ,  Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia Aki ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani

发明人： Purakkattle Biju ,  Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia Aki ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani

IPC分类号： A61K31/433 ,  A61K31/496 ,  A61K31/5377 ,  A61P19/00 ,  A61P25/00 ,  A61P3/00 ,  A61P37/00 ,  A61P9/00 ,  C07D285/10 ,  C07D417/10 ,  C07D417/14

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

摘要翻译： 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病，例如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：US07338968B2

公开(公告)日：2008-03-04

申请号：US11013753

申请日：2004-12-16

申请人： Purakkattle J. Biju ,  Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia J. Aki

发明人： Purakkattle J. Biju ,  Arthur G. Taveras ,  J. Robert Merritt ,  John J. Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia J. Aki

IPC分类号： C07D285/10 ,  A61K31/433

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

摘要翻译： 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病，例如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：US20060223864A1

公开(公告)日：2006-10-05

申请号：US11013753

申请日：2004-12-16

申请人： Purakkattle Biju ,  Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia Aki ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani

发明人： Purakkattle Biju ,  Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Younong Yu ,  Junying Zheng ,  Jianhua Chao ,  Cynthia Aki ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani

IPC分类号： A61K31/4439 ,  A61K31/433 ,  C07D417/02

CPC分类号： C07D285/10 ,  C07D285/06 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

摘要翻译： 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病，例如癌症，血管生成，血管生成性眼部疾病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和缺血再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：US20060025453A1

公开(公告)日：2006-02-02

申请号：US11017505

申请日：2004-12-20

申请人： Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Junying Zheng ,  Purakkattle Biju ,  Younong Yu ,  Jianhua Chao ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani ,  Gaifa Lai ,  Minglang Wu

发明人： Arthur Taveras ,  J. Merritt ,  John Baldwin ,  Junying Zheng ,  Purakkattle Biju ,  Younong Yu ,  Jianhua Chao ,  Jay Fine ,  Daniel Lundell ,  Tony Priestley ,  Angelo Reggiani ,  Gaifa Lai ,  Minglang Wu

IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/425 ,  C07D417/14

CPC分类号： C07D275/03 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

摘要翻译： 公开了下式的新化合物及其药学上可接受的盐和溶剂合物。 D和E是不同的组，其中一个是N，另一个是CR 50。 包含取代基A的基团的实例包括杂芳基，芳基，杂环烷基，环烷基，芳基，炔基，烯基，氨基烷基，烷基或氨基。 包含取代基B的基团的实例包括芳基和杂芳基。 还公开了治疗趋化因子介导的疾病如癌症，血管生成，血管生成性眼病，肺部疾病，多发性硬化，类风湿性关节炎，骨关节炎，中风和心脏再灌注损伤，疼痛（例如急性疼痛，急性和慢性 炎性疼痛和神经性疼痛），使用式IA化合物。

公开(公告)号：US09676780B2

公开(公告)日：2017-06-13

申请号：US14655572

申请日：2013-12-20

申请人： MERCK SHARP & DOHME CORP. ,  Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

发明人： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

摘要： Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.